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抑制剂/激活剂

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凋亡与自噬

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COH29 RNR Inhibitor COH29

COH29 (RNR Inhibitor COH29) 是一种高效，具有抗癌活性的核糖核苷酸还原酶 (RNR) 抑制剂。抑制核糖核苷酸还原酶的 IC50 为 16 μM。

货号：
TK0257
规格：

1mg
价格：
￥0.00

产品参数

CAS No.	1190932-38-7
生物活性	COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
分子式	C22H16N2O5S
分子量	420.44
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (118.92 mM; Need ultrasonic)
体内研究	COH29 results in a dose-dependent inhibition of MOLT-4 tumor xenograft growth with twice-daily oral dosing at 50 mg/kg and 100 mg/kg, which is pronounced by Day 12 of treatment. Similarly, 7 days of treatment of mice bearing TOV11D xenografts with 200, 300, or 400 mg/kg/day COH29 results in a dose-dependent inhibition of tumor xenograft growth. Tumor growth is significantly inhibited compared with the control group.
体外研究	COH29 (RNR Inhibitor COH29) overcome hydroxyurea and gemcitabine resistance in cancer cells. It effectively inhibits proliferation of most cell lines in the NCI 60 human cancer panel, most notably ovarian cancer and leukemia, but exerts little effect on normal fibroblasts or endothelial cells. Site-directed mutagenesis, NMR and surface plasmon resonance biosensor studies confirm COH29 binding to the proposed ligand-binding pocket and offer evidence for assembly blockade of the RRM1-RRM2 quaternary structure.
文献	•Cancers (Basel). 2021 Aug 20;13(16):4200. •Sci Rep. 2021 Jun 29;11(1):13474.
纯度及产品资料	98%

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